RXH-Reactive ¹⁸F-Vinyl Sulfones as Versatile Agents for PET Probe Construction

Efficient radiolabeling reactions are important chemical tools in biomedical research especially in probe construction. Herein, three ¹⁸F-labeled vinyl sulfones were prepared. In particular, ¹⁸F-PEG1-VS (((2-(2-(fluoro-¹⁸F)ethoxy)ethyl)sulfonyl)ethane) could not only allow chemoselective labeling of bioactive molecules containing -XH (X = S, NH) groups, but also react with red blood cells both in vitro and in living mice for potential cell tracking applications. In addition, these hydrophilic agents were found to cross the blood brain barrier (BBB) efficiently and localize at the cerebellum region. In summary, ¹⁸F-labeled vinyl sulfones provide a versatile platform for PET probe construction.